125138-08-1Relevant articles and documents
Cyclopropyl-spiro-piperidines useful as sodium channel blockers
Blass, Benjamin
, p. 697 - 698 (2012/11/13)
Voltage-gated ion channels are critical to the generation and propagation of electrical signals and action potentials in neuronal and muscle tissue. The voltage-gated sodium channels in particular mediate the rapid depolarization of cells, creating the rising phase of an action potential, which in turn activates voltage-gated calcium and potassium channels. To date, nine voltage-gated sodium channel subtypes have been identified, and blockers of these channels have been developed as antiarrhythmic agents, anticonvulsants, antiepileptics, and local anesthetics. Voltage-gated sodium channels have also been targeted for the treatment of neuropathic pain, as it has been established that these channels play a critical role in the nerve cells associated with this condition. Specifically, it has been hypothesized that neuropathic pain is a result of increased sodium channel activity in injured nerves and that selective blockade of sodium channels such as Nav1.7 would provide therapeutic relief. The present application describes a series of cyclopropyl-spiro-piperidines useful as sodium channel blockers for the treatment of chronic and neuropathic pain.
